OBJECTIVE: The objective of this study is to evaluate the anti-cancer potential of the novel class of quinazoline tethered acetamide derivatives against six different cancer cell lines.
METHOD: A novel series of various substituted quinazolinone acetamides were synthesized through a feasible scheme. The synthetic scheme involves the conversion of benzoxazinone (from anthranilic acid and benzoyl chloride) intermediate to 3-amino quinazoline-4-one which is further converted to the final amide by tethering with the propionyl chloride employing Schotten-Baumann Reaction conditions. All the synthesized derivatives characterized by IR, 1HNMR and MASS spectral methods and anti-cancer activity evaluated by employing MTT assay for six cancer cell lines and one normal human cell line.
RESULTS: All the synthesized compounds were screened for anti-cancer activity against six cancer cell lines, including A 549 (lung), DU 145 (prostate), HT 29 (colon), MCF-7 (breast), SiHA (cervical), B16F10 (mouse skin melanoma) and one normal human fibroblast cell lines. All the compounds displayed a decent cytotoxicity profile when compared with the standard drug, doxorubicin. Among the synthesized compounds (5a to 5n) tested, two compounds, 5f and 5g have demonstrated excellent cytotoxicity against SiHA and MCF-7 cancer cell lines.
CONCLUSION: Comparatively, most of the compounds displayed decent cytotoxicity potential relative to the standard drug, doxorubicin. Further investigations are needed to establish the detailed mechanism of action of the developed novel quinazolinone acetamides.
RESULTS: The rumen pH and concentration of propionate were greater (P
RESULTS: The key volatile compounds and aroma profile of six pineapple varieties grown in Malaysia were investigated by gas chromatography-olfactometry (GC-O), gas-chromatography-mass spectrometry and qualitative descriptive sensory analysis. A total of 59 compounds were determined by GC-O and aroma extract dilution analysis. Among these compounds, methyl-2-methylbutanoate, methyl hexanoate, methyl-3-(methylthiol)-propanoate, methyl octanoate, 2,5-dimethyl-4-methoxy-3(2H)-furanone, δ-octalactone, 2-methoxy-4-vinyl phenol, and δ-undecalactone contributed greatly to the aroma quality of the pineapple varieties, due to their high flavour dilution factor. The aroma of the pineapples was described by seven sensory terms as sweet, floral, fruity, fresh, green, woody and apple-like.
CONCLUSION: Inter-relationship between the aroma-active compounds and the pineapples revealed that 'Moris' and 'MD2' covaried majorly with the fruity esters, and the other varieties correlated with lesser numbers of the fruity esters. Hierarchical cluster analysis (HCA) was used to establish similarities among the pineapples and the results revealed three main groups of pineapples.